Functionally Selective Ligands for Study and Inhibition of Inflammation

Background: Due to the complexity of the complement system cascade, biological roles of many signaling receptors are unknown. Additionally, biased ligand binding to cell-bound receptors may lead to selective intracellular effector binding and ligand-specific pathway activation and function. Mechanistic knowledge forms the basis for assay development to explore pharmacology against complement-mediated inflammatory diseases. Brief Description: A multidisciplinary team of researchers from UCR, Texas A&M, Sheffield, and Queensland have discovered the first functionally selective peptide ligands for a complement system receptor that is involved in inflammation. The peptides are functionally selective ligands of C5aR2 but not C5aR1 or C3aR, and they have been characterized in vitro and in vivo. These peptides are novel tools that can modulate the activity of the receptor in vitro and in vivo, and interrogate the function of the receptor and its implication in inflammatory diseases. Grace Yee grace.yee@ucr.edu 951-827-2212

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